Application of hydroxypropyl methylcellulose as a protective agent against magnesium stearate induced crystallization of amorphous itraconazole

被引：12

作者：

Demuth, B. ^{[1
]}

Galata, D. L. ^{[1
]}

Balogh, A. ^{[1
]}

Szabo, E. ^{[1
]}

Nagy, B. ^{[1
]}

Farkas, A. ^{[1
]}

Hirsch, E. ^{[1
]}

Pataki, H. ^{[1
]}

Vigh, T. ^{[2
]}

Mensch, J. ^{[2
]}

Verreck, G. ^{[2
]}

Nagy, Z. K. ^{[1
]}

Marosi, G. ^{[1
]}

机构：

[1] Budapest Univ Technol & Econ, Dept Organ Chem & Technol, Muegyet Rkp 3, H-1111 Budapest, Hungary

[2] Janssen Res & Dev, Turnhoutseweg 30, B-2340 Beerse, Belgium

来源：

EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES | 2018年 / 121卷

关键词：

Amorphous solid dispersion; Hydroxypropyl methylcellulose; Dissolution; Downstream processing; Roller compaction; Hydrogen bonding; SOLID DISPERSIONS; MOLECULAR-INTERACTIONS; SOLUBLE DRUGS; FIBER MATS; ELECTROSPUN; DISSOLUTION; NANOFIBERS; BIOAVAILABILITY; RELEASE; HYDROXYPROPYLMETHYLCELLULOSE;

D O I：

10.1016/j.ejps.2018.06.008

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

Itraconazole is a fungicide drug which has low bioavailability due to its poor water solubility. Amorphous solid dispersion (ASD) is a tool that has the potential to greatly increase the dissolution rate and extent of compounds. In this work, the dissolution of tablets containing the ASD of itraconazole with either hydroxypropyl methylcellulose (HPMC) or vinylpyrrolidone-vinyl acetate copolymer (PVPVA) was compared in order to find a formulation which can prevent the drug from the precipitation caused by magnesium stearate. Formulations containing the PVPVA-based ASD with HPMC included in various forms could reach 90% dissolution in 2 h, while HPMC-based ASDs could release 100% of the drug. However, HPMC-based ASD had remarkably poor grindability and low bulk density, which limited its processability and applicability. The latter issue could be resolved by roller compacting the ASD, which significantly increases the bulk density and the flowability of the powder blends used for tableting. This roller compaction step might be a base for the industrial application of HPMC-based, electrospun ASDs.

引用

页码：301 / 308

页数：8

共 34 条

[1] Functional materials by electrospinning of polymers [J].

Agarwal, Seema ;

Greiner, Andreas ;

Wendorff, Joachim H. .

PROGRESS IN POLYMER SCIENCE, 2013, 38 (06) :963-991

[2] Electroblowing and electrospinning of fibrous diclofenac sodium-cyclodextrin complex-based reconstitution injection [J].

Balogh, Attila ;

Horvathova, Timea ;

Fueloep, Zoltan ;

Loftsson, Thorsteinn ;

Harasztos, Anna Helga ;

Marosi, Gyoergy ;

Nagy, Zsombor K. .

JOURNAL OF DRUG DELIVERY SCIENCE AND TECHNOLOGY, 2015, 26 :28-34

[3] Melt-Blown and Electrospun Drug-Loaded Polymer Fiber Mats for Dissolution Enhancement: A Comparative Study [J].

Balogh, Attila ;

Farkas, Balazs ;

Farago, Kornel ;

Farkas, Attila ;

Wagner, Istvan ;

Van Assche, Ivo ;

Verreck, Geert ;

Nagy, Zsombor K. ;

Marosi, Gyoergy .

JOURNAL OF PHARMACEUTICAL SCIENCES, 2015, 104 (05) :1767-1776

[4] Plasticized Drug-Loaded Melt Electrospun Polymer Mats: Characterization, Thermal Degradation, and Release Kinetics [J].

Balogh, Attila ;

Dravavoelgyi, Gabor ;

Farago, Kornel ;

Farkas, Attila ;

Vigh, Tamas ;

Soti, Peter Lajos ;

Wagner, Istvan ;

Madarasz, Janos ;

Pataki, Hajnalka ;

Marosi, Gyoergy ;

Nagy, Zsombor Kristof .

JOURNAL OF PHARMACEUTICAL SCIENCES, 2014, 103 (04) :1278-1287

[5]

Carr R.L., 1965, Chem. Eng, V72, P163, DOI DOI 10.1016/J.JAEROSCI.2007.10.003

[6] Enhanced bioavailability and bioefficacy of an amorphous solid dispersion of curcumin [J].

Chuah, Ai Mey ;

Jacob, Bindya ;

Jie, Zhang ;

Ramesh, Subbarayan ;

Mandal, Shibajee ;

Puthan, Jithesh K. ;

Deshpande, Parag ;

Vaidyanathan, Vadakkanchery V. ;

Gelling, Richard W. ;

Patel, Gaurav ;

Das, Tapas ;

Shreeram, Sathyavageeswaran .

FOOD CHEMISTRY, 2014, 156 :227-233

[7] Investigation of Deteriorated Dissolution of Amorphous Itraconazole: Description of Incompatibility with Magnesium Stearate and Possible Solutions [J].

Demuth, B. ;

Galata, D. L. ;

Szabo, E. ;

Nagy, B. ;

Farkas, A. ;

Balogh, A. ;

Hirsch, E. ;

Pataki, H. ;

Rapi, Z. ;

Bezur, L. ;

Vigh, T. ;

Verreck, G. ;

Szalay, Z. ;

Demeter, A. ;

Marosi, G. ;

Nagy, Z. K. .

MOLECULAR PHARMACEUTICS, 2017, 14 (11) :3927-3934

[8] Development and tableting of directly compressible powder from electrospun nanofibrous amorphous solid dispersion [J].

Demuth, B. ;

Farkas, A. ;

Szabo, B. ;

Balogh, A. ;

Nagy, B. ;

Vago, E. ;

Vigh, T. ;

Tinke, A. P. ;

Kazsu, Z. ;

Demeter, A. ;

Bertels, J. ;

Mensch, J. ;

Van Dijck, A. ;

Verreck, G. ;

Van Assche, I. ;

Marosi, G. ;

Nagy, Z. K. .

ADVANCED POWDER TECHNOLOGY, 2017, 28 (06) :1554-1563

[9] Detailed stability investigation of amorphous solid dispersions prepared by single-needle and high speed electrospinning [J].

Demuth, B. ;

Farkas, A. ;

Pataki, H. ;

Balogh, A. ;

Szabo, B. ;

Borbas, E. ;

Soti, P. L. ;

Vigh, T. ;

Kiserdei, E. ;

Farkas, B. ;

Mensch, J. ;

Verreck, G. ;

Van Assche, I. ;

Marosi, G. ;

Nagy, Z. K. .

INTERNATIONAL JOURNAL OF PHARMACEUTICS, 2016, 498 (1-2) :234-244

[10] Lubricant-Induced Crystallization of Itraconazole From Tablets Made of Electrospun Amorphous Solid Dispersion [J].

Demuth, Balazs ;

Farkas, Attila ;

Balogh, Attila ;

Bartosiewicz, Karolina ;

Kallai-Szabo, Barnabas ;

Bertels, Johny ;

Vigh, Tamas ;

Mensch, Jurgen ;

Verreck, Geert ;

Van Assche, Ivo ;

Marosi, Gyorgy ;

Nagy, Zsombor K. .

JOURNAL OF PHARMACEUTICAL SCIENCES, 2016, 105 (09) :2982-2988

← 1 2 3 4 →